Identification of Potential Therapeutics to Conquer Drug Resistance in Salmonella typhimurium: Drug Repurposing Strategy

Balasundaram, Preethi; Shanthi, V.; Ramanathan, K.

doi:10.1007/s40259-016-0200-7

Cited by 9 publications

(6 citation statements)

References 48 publications

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“…[a] BJH method; [b] BET specific areas; [c] P/P 0 = 0.9; [d] ICP analysis. no bulk SnO 2 particles were formed, [30] which was consistent with the XRD results. The peak at 210 nm can be obviously observed for the two samples, indicating that the tin species can been tetrahedrally incorporated into the skeleton of SnÀ Ti submicrospheres.…”

Section: Samplessupporting

confidence: 87%

“…The peak at 210 nm can be obviously observed for the two samples, indicating that the tin species can been tetrahedrally incorporated into the skeleton of SnÀ Ti submicrospheres. [30] However, compared to MTS-W-1.3 sample, the slight red shift of the maximum absorption peak edge for the MTS-W-4.0 sample was happened, which may be due to the reduction of band gap energy caused by the partial transformation into rutile phase from anatase phase. [31] XPS spectra for MTS-W-4.0 sample were shown in Figure 7.…”

Section: Samplesmentioning

confidence: 86%

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Sn‐Ti Submicrospheres with Tunable Particle Size for Cyclohexanone Baeyer‐Villiger Oxidation

Zhou

Sun

et al. 2022

ChemistrySelect

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Sn-Ti submicrospheres with tunable particle size were successfully synthesized by adjusting the water amount over Polyvinylpyrrolidone(PVP)-assisted sol-gel method in this paper, and the effect of the submicrosphere size on the catalytic performance in the B-V oxidation of cyclohexanone by molecular oxygen was also investigated. Their physical and chemical properties were character-rized by Scanning electron microscope (SEM), X-ray diffraction (XRD), N 2 sorption, Pyridineadsorbed IR(Py-IR), Uvioletvisible diffuse reflection spectroscopy(UV-vis), X-ray photoelectron spectra (XPS), Transmission electron microscope and Energy dispersive X-ray detector(TEM-EDX) techniques. The characterization results showed that the Sn-Ti crystal phase would be affected by the initial water amount resulting in the variation for the incorporation of tin species into the tetrahedral TiO 2 . The regular Sn-Ti submicrospheres with particle size about 210 � 5 nm and typical Lewis acidities for MTS-W-4.0 sample can be obtained when water amount was as high as 4.0 mL, and it exhibited higher catalytic performance than other catalysts where its εcaprolactone yield was 97.8 %. Compared to the decline range of 13.6 % with the submicrospheres particle size as about 450 nm, the drop of ε-caprolactone yield was only 3.9 % and the yield of ε-caprolactone can be kept at 93.9 % over MTS-W-4.0 sample after repeated use for 5 times.

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Section: Samplessupporting

confidence: 87%

Section: Samplesmentioning

confidence: 86%

Sn‐Ti Submicrospheres with Tunable Particle Size for Cyclohexanone Baeyer‐Villiger Oxidation

Zhou

Sun

et al. 2022

ChemistrySelect

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“…The imidazole derivatives-econazole and sulconazole- were developed mainly as antifungal drugs inhibiting fungal CYP450’s, leading to a decreased production of ergosterol, the essential bioregulator of fungal cell membrane fluidity and integrity 65–67 . The CYP-450 inhibitors, econazole and sulconazole, were found to display antiparasitic activity against Schistosoma mansoni 46 , antitrypanosomal activity 68 against Trypanosoma cruzi , and antibacterial activity against Mycobacterium tuberculosis 69 and against the drug resistant Salmonella typhimurium 70 . The antiparasitic activity of imidazoles is believed to act through their inhibitory activity against CYP-450’s that was recently found to be essential for the survival of protozoan and helminth parasites 46,50 and linked to the anthelmintic drug resistance 71 .…”

Section: Discussionmentioning

confidence: 99%

Drug Screening for Discovery of Broad-spectrum Agents for Soil-transmitted Nematodes

Elfawal

Savinov

Aroian

2019

Sci Rep

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Soil-transmitted nematodes (STNs), namely hookworms, whipworms, and ascarids, are extremely common parasites, infecting 1–2 billion of the poorest people worldwide. Two benzimidazoles, albendazole and mebendazole, are currently used in STN mass drug administration, with many instances of low/reduced activity reported. New drugs against STNs are urgently needed. We tested various models for STN drug screening with the aim of identifying the most effective tactics for the discovery of potent, safe and broad-spectrum agents. We screened a 1280-compound library of approved drugs to completion against late larval/adult stages and egg/larval stages of both the human hookworm parasite Ancylostoma ceylanicum and the free-living nematode Caenorhabditis elegans , which is often used as a surrogate for STNs in screens. The quality of positives was further evaluated based on cheminformatics/data mining analyses and activity against evolutionarily distant Trichuris muris whipworm adults. From these data, two pairs of positives, sulconazole/econazole and pararosaniline/cetylpyridinium, predicted to target nematode CYP-450 and HSP-90 respectively, were prioritized for in vivo evaluation against A . ceylanicum infections in hamsters. One of these positives, pararosaniline, showed a significant impact on hookworm fecundity in vivo . Taken together, our results suggest that anthelmintic screening with A . ceylanicum larval stages is superior to C . elegans based on both reduced false negative rate and superior overall quality of actives. Our results also highlight two potentially important targets for the discovery of broad-spectrum human STN drugs.

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“…For instance, the use of naproxen as a cytotoxic drug in urinary bladder cancer has been reported (Kim et al, 2014 ). Other repurposed applications have been proposed for meloxicam in the treatment of non-Hodgkin's lymphoma (Nugent et al, 2016 ; Chartier et al, 2017 ), etodolac for the treatment of breast cancer (Yang et al, 2014 ), tenoxicam for the treatment of tuberculosis (Maitra et al, 2016 ), hydrocortisone in the treatment of Alzheimer's Disease (Zhang et al, 2015 ), flufenamic acid for the treatment of Salmonella infection (Ekins et al, 2011 ; Preethi et al, 2016 ), fenoprofen as a melanocortin receptor allosteric enhancer (Montero-Melendez et al, 2017 ), and nabumetone (Shameer et al, 2017 ).…”

Section: Discussionmentioning

confidence: 99%

Exploration of the Anti-Inflammatory Drug Space Through Network Pharmacology: Applications for Drug Repurposing

et al. 2018

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The quintessential biological response to disease is inflammation. It is a driver and an important element in a wide range of pathological states. Pharmacological management of inflammation is therefore central in the clinical setting. Anti-inflammatory drugs modulate specific molecules involved in the inflammatory response; these drugs are traditionally classified as steroidal and non-steroidal drugs. However, the effects of these drugs are rarely limited to their canonical targets, affecting other molecules and altering biological functions with system-wide effects that can lead to the emergence of secondary therapeutic applications or adverse drug reactions (ADRs). In this study, relationships among anti-inflammatory drugs, functional pathways, and ADRs were explored through network models. We integrated structural drug information, experimental anti-inflammatory drug perturbation gene expression profiles obtained from the Connectivity Map and Library of Integrated Network-Based Cellular Signatures, functional pathways in the Kyoto Encyclopedia of Genes and Genomes (KEGG) and Reactome databases, as well as adverse reaction information from the U.S. Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS). The network models comprise nodes representing anti-inflammatory drugs, functional pathways, and adverse effects. We identified structural and gene perturbation similarities linking anti-inflammatory drugs. Functional pathways were connected to drugs by implementing Gene Set Enrichment Analysis (GSEA). Drugs and adverse effects were connected based on the proportional reporting ratio (PRR) of an adverse effect in response to a given drug. Through these network models, relationships among anti-inflammatory drugs, their functional effects at the pathway level, and their adverse effects were explored. These networks comprise 70 different anti-inflammatory drugs, 462 functional pathways, and 1,175 ADRs. Network-based properties, such as degree, clustering coefficient, and node strength, were used to identify new therapeutic applications within and beyond the anti-inflammatory context, as well as ADR risk for these drugs, helping to select better repurposing candidates. Based on these parameters, we identified naproxen, meloxicam, etodolac, tenoxicam, flufenamic acid, fenoprofen, and nabumetone as candidates for drug repurposing with lower ADR risk. This network-based analysis pipeline provides a novel way to explore the effects of drugs in a therapeutic space.

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Identification of Potential Therapeutics to Conquer Drug Resistance in Salmonella typhimurium: Drug Repurposing Strategy

Abstract: Overall, flufenamic acid and sulconazole may be potential drug candidates that could be studied in vitro to assess their resistance profile against Salmonella enterica Typhimurium.

Cited by 9 publications

References 48 publications

Sn‐Ti Submicrospheres with Tunable Particle Size for Cyclohexanone Baeyer‐Villiger Oxidation

Sn‐Ti Submicrospheres with Tunable Particle Size for Cyclohexanone Baeyer‐Villiger Oxidation

Drug Screening for Discovery of Broad-spectrum Agents for Soil-transmitted Nematodes

Exploration of the Anti-Inflammatory Drug Space Through Network Pharmacology: Applications for Drug Repurposing

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